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  3. Y134

Y134 

Cat. No.: HY-103457
Handling Instructions

Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells.

For research use only. We do not sell to patients.

Y134 Chemical Structure

Y134 Chemical Structure

CAS No. : 849662-80-2

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Description

Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells[1].

IC50 & Target[1]

ERα

0.09 nM (Ki)

ERβ

11.31 nM (Ki)

In Vitro

Y134 exhibits potent antagonist activity at ERs in CV-1 cells cotransfected with plasmids containing ERα or ERβ and oestrogen-response element-driven luciferase, with IC50[1].
Y134 (0.01 nM-10 μM; 6 d) inhibits the oestrogen-stimulated ER-expressing breast cancer cell (MCF-7 and T47D) proliferation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MCF-7, T47, MDA-MB-231 cells
Concentration: 0.01 nM-10 μM
Incubation Time: 6 days
Result: Suppressed oestrogen-stimulated MCF-7 and T47D cell proliferation.
Showed no effects on MDA-MB-231 cells, except some cytotoxicity was seen at high concentrations.
In Vivo

Y134 (1-3 mg/kg/day; p.o. for 3 days) abolishes the E2-induced mammary gland terminal end bud (TEB) outgrowth in ovariectomized rats. Y134 inhibits uterine cell proliferation induced by E2 in a dose-dependent manner[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four-week old female Sprague-Dawley rats were received ovariectomy[1]
Dosage: 1, 3 mg/kg
Administration: P.o. daily for 3 days
Result: Abolished the effect exerted by E2 in a dose-dependent manner.
Molecular Weight

472.60

Formula

C₂₈H₂₈N₂O₃S

CAS No.
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Y134
Cat. No.:
HY-103457
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